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Browsing by Author "Egan, Timothy J"

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The crystal structure of halofantrine–ferriprotoporphyrin IX and the mechanism of action of arylmethanol antimalarials.

Author: de Villiers, Katherine A ; Marques, Helder ; Egan, Timothy J Date: 2008 The crystal structure of the complex formed between the antimalarial drug halofantrine and ferriprotoporphyrin IX (Fe(III)PPIX) has been determined by single crystal X-ray diffraction. The structure shows that halofantrine coordinates to the ... Read more
Crystallization of calcium oxalate on molecularly imprinted polymer surfaces

Author: Tewolde, Tewolde Siele Date: 2004 Calcium oxalate (CaOx) is the most common component of human kidney stones. Heterogeneous nucleation is regarded as the key mechanism in this process. As such, crystallization of this substance has been studied in several different model ... Read more
Crystallization of synthetic haemozoin (beta-haematin) nucleated at the surface of lipid particles

Author: Hoang, Anh N ; Ncokazi, Kanyile K ; de Villiers, Katherine A ; Wright, David W ; Egan, Timothy J Date: 2010 The mechanism of formation of haemozoin, a detoxification by-product of several blood-feeding organisms including malaria parasites, has been a subject of debate; however, recent studies suggest that neutral lipids may serve as a catalyst. ... Read more
The design and synthesis of new transition metal coordination complexes as potential anti-malarial agents

Author: Hager, Emma Date: 2011 New Rh(I), Rh(III), Ir(III) and Pd(II) coordination complexes bearing 1,10-phenanthroline (phen) or 2,2'-bipyridyl (bipy) ligands have been investigated for potential anti-malarial activity. Read more
Development of quinoline and non-quinoline based organometallic complexes and their ligands conjugated to polyamine scaffolds as pharmacological agents

Author: Stringer, Tameryn Date: 2014 Malaria remains a major global health problem and to date, hundreds of thousands of people die as a result of this disease every year. Malaria has been able to adapt and rebound despite various efforts made to combat the disease. The decrease ... Read more
Discovery of benzamides and triarylimidazoles active against Plasmodium falciparum via haemozoin inhibition : high throughput screening, synthesis and structure-activity relationships

Author: Wicht, Kathryn Jean Date: 2015 New antimalarials are desperately needed to overcome growing P. falciparum resistance to the current drugs. Successful quinoline-based drugs target haemozoin formation causing a cytotoxic accumulation of free haem (Fe(III)PPIX) in the parasite, ... Read more
Experimental and time-dependent density functional theory characterization of the UV−Visible spectra of monomeric and μ‑Oxo dimeric ferriprotoporphyrin IX

Author: Kuter, David ; Venter, Gerhard A ; Naidoo, Kevin J ; Egan, Timothy J Date: 2012 Speciation of ferriprotoporphyrin IX, Fe(III)PPIX, in aqueous solution is complex. Despite the use of its characteristic spectroscopic features for identification, the theoretical basis of the unique UV−visible absorbance spectrum of μ- ... Read more
Haematin-Quinoline interactions and structure-activity relationships in the antimalarial chloroquine and related compounds

Author: Kaschula, Catherine Hart Date: 2002 The nature of the ferriprotoporphyrin IX (Fe(III)PPIX) antimalarial drug target and its interactions with aminoquinolines was investigated spectrophotometrically. The antiquity of malaria, which is caused by protozoan parasites of the genus ... Read more
Haemozoin formation

Author: Egan, Timothy J Date: 2008 Formation of malaria pigment or haemozoin is the major route of haem detoxification in the malaria parasite Plasmodium falciparum as well as several other species of haematophagous organisms, including other Plasmodium species, helminth worms ... Read more
Increase on the initial soluble heme levels in acidic conditions is an important mechanism for spontaneous heme crystallization in vitro

Author: Stiebler, Renata ; Hoang, Anh N ; Egan, Timothy J ; Wright, David W ; Oliveira, Marcus F Date: 2010 BACKGROUND: Hemozoin (Hz) is a heme crystal that represents a vital pathway for heme disposal in several blood-feeding organisms. Recent evidence demonstrated that β-hematin (βH) (the synthetic counterpart of Hz) formation occurs under ... Read more c b
Insights into the mechanism of action of quinoline antimalarials against Plasmodium falciparum revealed by novel fluorescent analogues and chemical proteomics

Author: Woodland, John Geoffrey Date: 2016 For centuries, quinoline-based drugs have formed the cornerstone of antimalarial treatment. Despite recent challenges posed by resistance, interest in these molecules persists. It is thus surprising that crucial details of their mechanism of ... Read more
Interactions of quinoline antimalarials with haematin and their effect on ß-haematin formation

Author: Ncokazi, Kanyile K Date: 2005 Thermodynamic compensation in the interaction of quinoline antimalarials with haematin in 40% (v/v) aqueous OMSO has been compared with that in pure aqueous solution. The data indicate that the degree of desolvation and loss of conformational ... Read more
Interplay between Plasmodium falciparum haemozoin and l-arginine: implication for nitric oxide production

Author: Corbett, Yolanda ; D’Alessandro, Sarah ; Parapini, Silvia ; Scaccabarozzi, Diletta ; Kalantari, Parisa ; Zava, Stefania ; Giavarini, Flavio ; Caruso, Donatella ; Colombo, Irma ; Egan, Timothy J ; Basilico, Nicoletta Date: 06 Dec 2018 Abstract Background Plasmodium falciparum haemozoin, a detoxification product of digested haemoglobin from infected erythrocytes, is released into the bloodstream upon schizont rupture and ... Read more
Investigating the structure-function relationships of Plasmodium Haem Detoxification Protein and Phosphatidylinositol 4-kinase

Author: Wambua, Lynn Date: 2022 The human malaria parasite Plasmodium falciparum relies on proteins and protein-mediated processes to survive, replicate in the host and evade the host's immune response. This study focuses on two Plasmodium proteins: (i) Haem Detoxification ... Read more
Kinetics of β-haematin formation in benzoic acid

Author: Tshivhase, Mmboneni Gifty Date: 2005 Haemozoin is a cyclic dimer of ferriprotoporphyrin (IX) that occurs in malariaparasites and some other blood-eating organisms. It is chemically identical to β-haematin. In this work, the kinetics of β-haematin formation were investigated in ... Read more
The mechanism of beta-hematin formation in acetate solution. Parallels between hemozoin formation and biomineralization processes

Author: Egan, Timothy J ; Mavuso, Winile W ; Ncokazi, Kanyile K Date: 2001 Formation of â-hematin in acidic acetate solution has been investigated using quantitative infrared spectroscopy, X-ray diffraction, and scanning and transmission electron microscopy. The process occurs via rapid precipitation of amorphous ... Read more
Physicochemical, biological and β-haematin inhibiting activity of pyrido-dibemequines, pyrido[1,2-α]benzimidazoles and their derivatives

Author: Okombo, Ojwang' John Date: 2018 There is an urgent need for new antimalarials following the emergence of Plasmodium falciparum strains with reduced sensitivity to the currently used artemisinin combination therapies. Classical aminoquinoline-based drugs inhibit the formation ... Read more
Quinoline antimalarials decrease the rate of beta-hematin formation

Author: Egan, Timothy J ; Ncokazi, Kanyile K Date: 2005 The strength of inhibition of b-hematin (synthetic hemozoin or malaria pigment) formation by the quinoline antimalarial drugs chloroquine, amodiaquine, quinidine and quinine has been investigated as a function of incubation time. In the assay ... Read more c b n d
The role of haem in the mechanism of action of antimalarials in Plasmodium falciparum

Author: Combrinck, Jill Michelle Date: 2016 The malaria parasite detoxifies host red blood cell derived haem by conversion into the inert biocrystal haemozoin. Inhibiting this critical pathway is proposed to be the mechanism of action of chloroquine and related antimalarials and several ... Read more
The role of lipid in malaria pigment (Haemozoin) formation under biomimetic conditions

Author: Ambele, Melvin Anyasi Date: 2013 Previous studies have proposed lipids and/or proteins to be involved in the biomineralization process of haemozoin formation in the malaria parasite which is a target for many antimalarial drugs. This study therefore investigated the biomolecules ... Read more

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